ledipasvir [Ligand Id: 11271] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2374220 (GS-5885, Ledipasvir, Ledipasvir acetonate)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Nonstructural protein 5A in Hepatitis C virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3307224] [UniProtKB: Q5L478]
ChEMBL Inhibition of NS5A in HCV genotype 3a by cell based luciferase reporter gene assay B 7.39 pIC50 41 nM IC50 J Med Chem (2019) 62: 10563-10582 [PMID:31710479]
ChEMBL Inhibition of NS5A in HCV genotype 2a JFH-1 by cell based luciferase reporter gene assay B 7.68 pIC50 21 nM IC50 J Med Chem (2019) 62: 10563-10582 [PMID:31710479]
ChEMBL Inhibition of NS5A R44K mutant in HCV genotype 2b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.03 pEC50 943 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 2b MD2b-1 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.06 pEC50 865 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 2b MD2b-1 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.28 pEC50 530 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A P58S mutant in HCV genotype 2b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.53 pEC50 292 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 6e D88 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.58 pEC50 264 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 2a J6 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.6 pEC50 249 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A N62V mutant in HCV genotype 2a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.65 pEC50 222 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 2b AY232738 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.68 pEC50 211 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV wild type genotype 2a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.68 pEC50 209 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Q30E mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.77 pEC50 169 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 3a S52 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.77 pEC50 168 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A K44R mutant in HCV genotype 2a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.79 pEC50 164 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A N62S mutant in HCV genotype 2a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 6.91 pEC50 123 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A A30K mutant in HCV genotype 3a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.05 pEC50 >88.8 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93H mutant in HCV genotype 3a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.05 pEC50 >88.8 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93H mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.28 pEC50 52 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93C mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.3 pEC50 49.6 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 3a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.35 pEC50 >44.8 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 2a JFH1 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Q30R mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.71 pEC50 19.6 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A L31M mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 7.77 pEC50 17 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93H mutant in HCV genotype 1b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 8.14 pEC50 7.2 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Q30H mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 8.24 pEC50 5.7 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A M28T mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 8.72 pEC50 1.9 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 6a HK6 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 8.96 pEC50 1.1 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 4a ED43 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.41 pEC50 0.39 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 5a SA13 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.82 pEC50 0.15 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.51 pEC50 0.03 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.51 pEC50 0.03 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]